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Entecavir monohydrate

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Catalog No. T0085Cas No. 209216-23-9
Alias SQ 34676, Entecavir hydrate, BMS-200475

Entecavir monohydrate (BMS-200475) is a selective inhibitor of the replication of the hepatitis B virus (HBV). It, a new deoxyguanine nucleoside analog.

Entecavir monohydrate

Entecavir monohydrate

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Purity: 99.73%
Catalog No. T0085Alias SQ 34676, Entecavir hydrate, BMS-200475Cas No. 209216-23-9
Entecavir monohydrate (BMS-200475) is a selective inhibitor of the replication of the hepatitis B virus (HBV). It, a new deoxyguanine nucleoside analog.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$30In StockIn Stock
5 mg$44In StockIn Stock
10 mg$77In StockIn Stock
25 mg$116In StockIn Stock
50 mg$162In StockIn Stock
100 mg$243In StockIn Stock
1 mL x 10 mM (in DMSO)$48In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.73%
Color:White
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Product Introduction

Bioactivity
Description
Entecavir monohydrate (BMS-200475) is a selective inhibitor of the replication of the hepatitis B virus (HBV). It, a new deoxyguanine nucleoside analog.
Targets&IC50
HBV (HepG2 cells):3.75 nM(ec50)
In vitro
In ducks, Entecavir administration results in a 4-log reduction of serum DHBV DNA levels within 80 days and a 2- to 3-log decrease in hepatitis B virus surface antigen within 120 days. Treatment with Entecavir also decreases replication intermediates of DHBV DNA in the liver by a factor of 70, while covalently closed circular DNA levels are only reduced fourfold under stable template conditions. Additionally, Entecavir reduces both the intensity of antigen staining and the percentage of antigen-positive cells in the liver, although there is an increase in antigen staining intensity in bile duct cells.
In vivo
In liver biopsy samples, Entecavir reduces both covalently closed circular DNA and the negativity of the hepatitis B virus core antigen. Entecavir triphosphate acts as an effective inhibitor of the wild-type HBV polymerase and is 100-300 times more potent than lamivudine triphosphate against 3TC-resistant HBV polymerase. To inhibit the replication of 3TC-resistant HBV, Entecavir requires a concentration that is 20-30 times higher. With an EC50 of 0.1 nM, Entecavir demonstrates significant activity against HIV. It can be utilized in a single-cycle, single-cell line pseudovirus assay, measuring green fluorescent protein in CD4+ lymphocytes using fluorescence-activated cell sorting.
Cell Research
BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×105 cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10[1].
SynonymsSQ 34676, Entecavir hydrate, BMS-200475
Chemical Properties
Molecular Weight295.3
FormulaC12H15N5O3·H2O
Cas No.209216-23-9
SmilesO.Nc1nc(=O)c2ncn([C@H]3C[C@H](O)[C@@H](CO)C3=C)c2[nH]1
Relative Density.1.81
Storage & Solubility Information
Storagekeep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (186.25 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (8.47 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.3864 mL16.9319 mL33.8639 mL169.3193 mL
5 mM0.6773 mL3.3864 mL6.7728 mL33.8639 mL
10 mM0.3386 mL1.6932 mL3.3864 mL16.9319 mL
20 mM0.1693 mL0.8466 mL1.6932 mL8.4660 mL
50 mM0.0677 mL0.3386 mL0.6773 mL3.3864 mL
100 mM0.0339 mL0.1693 mL0.3386 mL1.6932 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
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μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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